GSK1702934A


Catalog No. Size PriceQuantity
M13460-2 2mg solid $125
M13460-10 10mg solid $375

Description

GSK1702934A is a selective TRPC3 agonist. GSK1702934A modulates cardiac contractility and f arrhythmogenesis by activation of TRPC3.

Product information

CAS Number: 924377-85-5

Molecular Weight: 395.52

Formula: C22H25N3O2S

Chemical Name: 1-(1-{4H,5H,6H,7H,8H-cyclohepta[b]thiophene-2-carbonyl}piperidin-4-yl)-2,3-dihydro-1H-1,3-benzodiazol-2-one

Smiles: O=C1NC2=CC=CC=C2N1C1CCN(CC1)C(=O)C1=CC2CCCCCC=2S1

InChiKey: AXWRAIIIBRLXBP-UHFFFAOYSA-N

InChi: InChI=1S/C22H25N3O2S/c26-21(20-14-15-6-2-1-3-9-19(15)28-20)24-12-10-16(11-13-24)25-18-8-5-4-7-17(18)23-22(25)27/h4-5,7-8,14,16H,1-3,6,9-13H2,(H,23,27)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (252.83 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

GSK1702934A is able to induce TRPC3/6-currents in HEK293 cells transduced with recombinant human TRPC3/6 with an EC50 of 0.08 mM and 0.44 mM, respectively. GSK1702934A induces a transient, non-selective conductance and prolonged action potentials in TRPC3-overexpressing myocytes but not in wild-type myocytes. GSK1702934A substantially promotes NCX currents in TRPC3-overexpressing myocytes.

In Vivo:

GSK1702934A (0.3-3 mg/kg; i.v.) transiently increases blood pressure by 15 ~ 35 mmHg in conscious Sprague Dawley rats.

References:

  1. de la Cruz GG, et al. Intensified Microwave-Assisted N-Acylation Procedure - Synthesis and Activity Evaluation of TRPC3 Channel Agonists with a 1,3-Dihydro-2H-benzo[d]imidazol-2-one Core. Synlett. 2017 Apr;28(6):695-700.
  2. Doleschal B, et al. TRPC3 contributes to regulation of cardiac contractility and arrhythmogenesis by dynamic interaction with NCX1. Cardiovasc Res. 2015 Apr 1;106(1):163-73.
  3. Xu, X., et al. Schnackenberg, C. G. Characterization of Small Molecule TRPC3 and TRPC6 agonist and Antagonists. Biophysical Journal, 2013. 104(2), 454a.

Products are for research use only. Not for human use.

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